Nephrotoxicity or renal toxicity can be a result of hemodynamic changes, direct injury to cells and tissue, inflammatory tissue injury, and/or obstruction of renal excretion. Nephrotoxicity is frequently induced by a wide spectrum of therapeutic drugs and environ mental pollutants. Knowledge of the complex molecular and pathophysiologic mechanisms leading to nephrotoxicity remains limited, in part, by research that historically focused on single or relatively few risk markers. As such, current kidney injury biomarkers are inadequate in terms of sensitivity and specificity. In contrast, metabolomics enables screening of a vast array of metabolites simultaneously using NMR and MS to assess their role in nephrotoxicity development and progression. A more comprehensive understanding of these biochemical pathways would also provide valuable insight to disease mechanisms critical for drug development and treatment.